title: Modifications of the isonipecotic acid fragment of SNS-032: analogs with improved permeability and lower efflux ratio.
abstract: Modifications of the isonipecotic acid fragment of SNS-032 results in analogs which are more permeable and lower effluxed than SNS-032. The enantiomerically pure synthesis and the in vivo profile of analog 20 is described.
authors.affiliation: Sunesis Pharmaceuticals, 341 Oyster Point Blvd, South San Francisco, CA 94080, USA. jfan@sunesis.com
authors.forename: Junfa
authors.initials: J
authors.lastname: Fan
authors.forename: Bruce
authors.initials: B
authors.lastname: Fahr
authors.forename: David
authors.initials: D
authors.lastname: Stockett
authors.forename: Erica
authors.initials: E
authors.lastname: Chan
authors.forename: Sravanthi
authors.initials: S
authors.lastname: Cheeti
authors.forename: Iana
authors.initials: I
authors.lastname: Serafimova
authors.forename: Yafan
authors.initials: Y
authors.lastname: Lu
authors.forename: Phuongly
authors.initials: P
authors.lastname: Pham
authors.forename: Duncan H
authors.initials: DH
authors.lastname: Walker
authors.forename: Ute
authors.initials: U
authors.lastname: Hoch
authors.forename: Ingrid C
authors.initials: IC
authors.lastname: Choong
mesh_terms: D000818:Animals; D020650:Combinatorial Chemistry Techniques; D051357:Cyclin-Dependent Kinase 2 / Q000037:antagonists & inhibitors*; D007540:Isonipecotic Acids / Q000737:chemistry* / Q000494:pharmacology; D051379:Mice; D015394:Molecular Structure; D010080:Oxazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D007540:Isonipecotic Acids; C484864:N-(5-(((5-(1,1-dimethylethyl)-2-oxazolyl)methyl)thio)-2-thiazolyl)-4-piperidinecarboxamide; D010080:Oxazoles; D013844:Thiazoles; D051357:Cyclin-Dependent Kinase 2